Receptors for Drugs: Discovery in the Post-Genomic Era

Authored by: Jeffrey M. Herz , William J. Thomsen

Encyclopedia of Pharmaceutical Science and Technology

Print publication date:  July  2013
Online publication date:  July  2013

Print ISBN: 9781841848198
eBook ISBN: 9781351124874
Adobe ISBN:


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A paradigm shift has occurred in receptor-based drug discovery based upon the elucidation of the complete human genome and advances in genomics research, which have revealed a plethora of potential new receptors on which to focus drug discovery efforts. Based on sequence, structural, and functional similarities of a great number of receptors, these receptor targets can be grouped into relatively few multigene superfamilies. Molecular biological approaches have also revealed that additional receptor subtypes and isoforms are generated through multiple mechanisms. The current challenge lies in the development and application of new strategies for rapidly mining the receptor genome sequences to establishing and understanding their function, which has been referred to as “functional genomics.” Practical problems and approaches to assays for the characterization of the ligand binding and elucidating signaling properties of expressed orphan receptors are critically evaluated. The ensuing characterization of orphan receptors is expected to reveal therapeutically important receptor targets that will serve as a platform for much of the drug discovery enterprise. These findings will spur the discovery and development of a new generation of receptor-subtype specific drugs with enhanced therapeutic specificity.

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